5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1989-94. doi: 10.1016/j.bmcl.2012.01.034. Epub 2012 Jan 21.

Abstract

5-Aryl-4-carboxamide-1,3-oxazoles are a novel, potent and selective series of GSK-3 inhibitors. The optimization of the series to yield compounds with cell activity and brain permeability is described.

MeSH terms

  • Animals
  • Bipolar Disorder / drug therapy
  • Brain / metabolism
  • Glycogen Synthase Kinase 3 / antagonists & inhibitors*
  • Glycogen Synthase Kinase 3 / metabolism
  • Humans
  • Models, Molecular
  • Oxazoles / chemical synthesis
  • Oxazoles / chemistry*
  • Oxazoles / pharmacokinetics
  • Oxazoles / pharmacology*
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacokinetics
  • Protein Kinase Inhibitors / pharmacology*
  • Rats
  • Structure-Activity Relationship

Substances

  • Oxazoles
  • Protein Kinase Inhibitors
  • Glycogen Synthase Kinase 3